BRL54443

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BRL54443 是一种有效的、相对选择性的 5-HT1E/1F 激动剂，Ki 分别为 2/1 nM。

BRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively; shows low affinity for other receptors 5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM); selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production with IC50 of 14 nM in DG membranes; significantly reduces formalin-induced flinching in rats.

Despite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50=14 nM). BRL 54443 also induces contraction (-log EC50=6.52).

Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.

BRL 54443 | BRL-54443

Endocrinology/Hormones

5-HT Receptor

5-HT1A|5-HT1B|5-HT1D|5-HT1E|5-HT1F

Cardiovascular Disease

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57477-39-1

230.3055

C14H18N2O

>98% (HPLC)

DMSO: ≥ 51 mg/mL

CN1CCC(C2=CNC3=C2C=C(O)C=C3)CC1

1H-Indol-5-ol, 3-(1-methyl-4-piperidinyl)-

(-20℃)

With Ice Pack

≥ 2 years